| 摘要 |
Aminoindazole derivatives (I), their racemates, enantiomers, diastereoisomers, mixtures, tautomers and their salts are new. Aminoindazole derivatives (I), their racemates, enantiomers, diastereoisomers, mixtures, tautomers and their salts are new. R3 = H, 1-6C alkyl, aryl, aryl alkyl, heteroaryl, heteroaryl alkyl, aryl or heteroaryl fused to 1-10C cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, or C(=NH)NR1 (all optionally substituted by one or more of halogen, CN, NO2, NH2, OH, OR1, COOH, COOR1, -O-CO-R1, NR1R2, NHCO-R1, CO-NR1R2, SR1, SO-R1, SO2R1, NHSO2-R1, SO2NR1R2, CS-NR1R2, NH-CS-R1, -O-SO2-R1, -SO2-O-R1, aryl, heteroaryl, formyl, oxo, trifluoromethyl, trifluoromethyl sulfanyl, trifluoromethoxy, and 1-6C alkyl); R5, R6, and R7 = halogen, CN, NO2, NH2, OH, OR8, COOH, COOR8, -O-CO-R8, NR8R9, NHCO-R8, CO-NR8R9, NH-CS-R8, CS-NR8R9, SR8, SO-R8, SO2R8, NHSO2-R8, SO2NR8R9, -O-SO2-R8, -SO2-O-R8, CF3, CF3O-, 1-6C alkyl or alkoxy, aryl, aryl alkyl, heteroaryl, heteroaryl alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl, polycycloalkyl (all optionally substituted by one or more of halogen, CN, NO2, NH2, OH, OR10, COOH, COOR10, -O-CO-R10, NR10R11, NHCO-R10, CO-NR10R11, NH-CS-R10, -CS-NR10R11, SR10, SO-R10, SO2R10, NHSO2R10, SO2NR10R11, -O-SO2-R10, -SO2-O-R10, aryl, heteroaryl, formyl, oxo, CF3, CF3O, and 1-6C alkyl); R1, R2, R8, R9, R10, and R11 = H, 1-6C alkyl, aryl, alkenyl, alkynyl, heteroaryl, cycloalkyl, or heterocycloalkyl (all optionally substituted by 1 or more halogen, alkyl, alkoxy, CN, NO2, NH2, OH, COOH, COOalkyl, CONH2, formyl, oxo, CF3, and CF3O); and provided that when R3 is 5-imidazolyl, 5-oxazolyl, 5-thiazolyl, 3-pyridinyl, or 5-pyrimidinyl, optionally substituted by halogen or alkyl, then at least one of R5, R6, and R7 is CN, NO2, NH2, OH, -O-CO-R8, NHCO-R8, NH-CS-R8, CS-NR8R9, NHSO2-R8, -O-SO2-R8, -SO2-O-R8, CF3, CF3O, alkoxy, aryl, arylalkyl, heteroaryl, heteroaryl alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl, or polycycloalkyl (all optionally substituted by halogen, CN, NO2, NH2, OH, OR10, COOH, COOR10, -O-CO-R10, NR10R11, NHCO-R10, CO-NR10R11, NH-CS-R10, -CS-NR10R11, SR10, SO-R10, SO2R10, NHSO2R10, SO2NR10R11, -O-SO2-R10, -SO2-O-R10, aryl, heteroaryl, formyl, oxo, CF3, CF3O, and 1-6C alkyl). Independent claims are also included for the following: (1) preparation of (I); and (2) 6,7-difluoro-1H-indazole-3-amine. N-(6,7-difluoro-1H-indazol-3-yl)butanamide, N-(6,7-difluoro-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)butanamide, N-(5-bromo-6,7-difluoro-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)butanamide, N-(6,7-difluoro-5-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)butanamide, 6,7-difluoro-5-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3-amine and N-(6,7-difluoro-5-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-3-yl)-N'-phenylurea as new intermediates in the preparation of (I). |
